This invention relates to 2-(substituted sulfamyl)-6-nitrobenzoic acids, esters, amides and N-substituted amides thereof used as sensitizers of hypoxic tumor cells to therapeutic radiation. It also relates to the process of preparing such compounds starting with a 2-chlorosulfonyl-6-nitro benzoate ester and aminating said 2-chlorosulfonyl benzoate ester to produce the corresponding 2-(substituted sulfamyl)-6-nitrobenzoic ester, and converting said ester to the substituted carboxamide.
At the present time, certain other unrelated compounds are in experimental clinical use as radiation sensitizers. However, these compounds--for example, metronidazole and misonidazole--suffer from the drawback that they also cause neurotoxicity which limits their usefulness. The compounds of the present invention are effective radiation sensitizers, and are believed to have a more favorable therapeutic ratio.